In Vivo Molecular Imaging by Positron Emission Tomography (PET) and its Application to Drug Design and Diagnosis

Abstract

Positron emission tomography (PET) is a powerful noninvasive method for molecular imaging in living systems, including the brain, heart, and other active tissues and organs. The need to develop new PET tracers has grown with the increase in use of this technique in biochemistry, medicine (diagnosis), and drug development. We here describe the overview of the recent advances and perspective in this interdisciplinary scientific area, focusing on current PET technology and new tracer synthesis particularly based on new methodologies for incorporating a short-lived ¹¹C-nuclide into bioactive organic molecules through Pd(0)-mediated rapid methylation and carbonylations. The former method has been applied to the synthesis of 15R-[¹¹C] TIC methyl ester, an efficient PET tracer for imaging a novel CNS-type prostacyclin receptor (IP₂) in living human brain.